Liu, Jingbao’s team published research in Pharmazie in 70 | CAS: 56503-96-9

Pharmazie published new progress about 56503-96-9. 56503-96-9 belongs to thiazole, auxiliary class Thiazole,Amine,Naphthalene, name is 4-(Naphthalen-1-yl)thiazol-2-amine, and the molecular formula is C13H10N2S, Name: 4-(Naphthalen-1-yl)thiazol-2-amine.

Liu, Jingbao published the artcileDesign, synthesis, and biological evaluation of 2-substituted ethenesulfonic acid ester derivatives as selective PTP1B inhibitors, Name: 4-(Naphthalen-1-yl)thiazol-2-amine, the publication is Pharmazie (2015), 70(7), 446-451, database is CAplus and MEDLINE.

Fifteen 2-substituted ethenesulfonic acid ester derivatives were designed, synthesized, and evaluated for the inhibitory activities against protein tyrosine phosphatase 1B (PTP1B) and T-Cell protein tyrosine phosphatase (TCPTP). The structural activity relationship (SAR) of these compounds were discussed to clarify the impact of the linker and the optimized tail on the inhibitory activity of PTP1B and selectivity over TCPTP. Most of the compounds exhibited excellent inhibitory activities against PTP1B with IC50 values of 1.5-8.9 μM. SAR anal. revealed that the substituents at the hydrophobic tail significantly alter the inhibitory activity against PTP1B and selectivity over TCPTP, e.g. compound Ethyl-2-(4-(3-(4-(2-chlorophenyl)thiazol-2-ylamino)propoxy)phenyl)ethenesulfonate showed excellent inhibitory activity to PTP1B with IC50 = 7.8 μM, and ∼6-fold selectivity over TCPTP. Combined with our previous findings, that the linker length and the substituted hydrophobic tail had decisive influence on the PTP1B inhibitory activity and selectivity was confirmed.

Pharmazie published new progress about 56503-96-9. 56503-96-9 belongs to thiazole, auxiliary class Thiazole,Amine,Naphthalene, name is 4-(Naphthalen-1-yl)thiazol-2-amine, and the molecular formula is C13H10N2S, Name: 4-(Naphthalen-1-yl)thiazol-2-amine.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica